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    GNE-049
    GNE-049

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V4551
    CAS #: 1936421-41-8Purity ≥98%

    Description: GNE-049 is a novel, highly potent and selective CBP/p300 bromodomain inhibitor with an IC50 of 1.1 nM in TR-FRET assay. GNE-049 also inhibits BRET and BRD4(1) with IC50s of 12 nM and 4200 nM, respectively. Inhibition of the bromodomain of the transcriptional regulator CBP/P300 is an especially interesting new therapeutic approach in oncology. It was discovered based on the in vivo chemical tool 1 (GNE-272) for the bromodomain of CBP that was moderately potent and selective over BRD4(1). In pursuit of a more potent and selective CBP inhibitor, we used structure-based design. Constraining the aniline of 1 into a tetrahydroquinoline motif maintained potency and increased selectivity 2-fold. Structure-activity relationship studies coupled with further structure-based design targeting the LPF shelf, BC loop, and KAc regions allowed us to significantly increase potency and selectivity, resulting in the identification of non-CNS penetrant 19 (GNE-781, TR-FRET IC50 = 0.94 nM, BRET IC50 = 6.2 nM; BRD4(1) IC50 = 5100 nΜ) that maintained good in vivo PK properties in multiple species. GNE-049 displays antitumor activity in an AML tumor model and was also shown to decrease Foxp3 transcript levels in a dose dependent manner.

    References:  2017 Nov 22;60(22):9162-9183.


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    GNE-049

    Name: GNE-049
    CAS#: 1936421-41-8
    Chemical Formula: C26H30F2N6O2
    Exact Mass: 496.2398
    Molecular Weight: 496.5628
    Elemental Analysis: C, 62.89; H, 6.09; F, 7.65; N, 16.92; O, 6.44
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Technical InformationSynonym: GNE-049; GNE 049; GNE049.
    IUPAC/Chemical Name: 1-[3-[7-(difluoromethyl)-6-(1-methylpyrazol-4-yl)-3,4-dihydro-2H-quinolin-1-yl]-1-tetrahydrofuran-3-yl-6,7-dihydro-4H-pyrazolo[4,3-c]pyridin-5-yl]ethanone
    InChi Key: FLTYKXCCCAPRLV-UHFFFAOYSA-N
    InChi Code: InChI=1S/C26H30F2N6O2/c1-16(35)32-8-5-23-22(14-32)26(30-34(23)19-6-9-36-15-19)33-7-3-4-17-10-20(18-12-29-31(2)13-18)21(25(27)28)11-24(17)33/h10-13,19,25H,3-9,14-15H2,1-2H3
    SMILES Code: CC(N1CCC(N(C2COCC2)N=C3N4CCCC5=C4C=C(C(F)F)C(C6=CN(C)N=C6)=C5)=C3C1)=O


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